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Abstract

The purpose of the research was to develop and evaluate metronidazole loaded HPMC K15M mucoadhesive microcapsules for sustained drug release at the gastric mucosa. Metronidazole mucoadhesive microcapsules were formulated by ion gelation technique using 3 2 factorial designs. A 3 2 full factorial designs were used to derive a statistical equation, ANOVA analysis, contour plots, and 3D response surface plots. Different polymer ratios of HPMC K15M and sodium alginate were used to formulate nine formulations (F1 to F9) of HPMC K15M loaded mucoadhesive microcapsules of metronidazole. In-vitro drug release and mucoadhesion were carried out by USP29 type-II tablet dissolution test apparatus and disintegration tester using goat stomach mucosa. The formulation was characterized by determining possible drug-polymer interaction using FT-IR, the percentage of yield, particle size, the percentage of entrapment efficiency, swelling index, the percentage of mucoadhesion and percentage of drug release. FT-IR spectroscopy result shows the interaction between the drug and polymers combined. The optimized formulations F9 exhibited high drug entrapment efficiency of 92.07 ± 0.02%, particle size of 852.46 ± 0.04 (μm), percentage yield of 96.36 ± 0.04%, swelling index of 99.25 ± 0.02%, percentage of mucoadhesion after 8 h was 69.00 ± 0.04%, and the drug release (49.70 ± 0.01%) sustained more than 14 h. Metronidazole mucoadhesive microcapsules adhered more strongly to gastric mucous layer and could retain in the gastric mucosa for an extended period, followed by a non-Fickian type of release. The study shows that metronidazole mucoadhesive microcapsules can be effectively used for sustained drug release to the gastric mucosa in the treatment of H. pylori infection.